JPH0427204B2 - - Google Patents

Description

[Detailed description of the invention]

[Industrial Field of Application] The present invention relates to an anti-caries and anti-periodontal composition containing an ethyl acetate soluble fraction of tea water or alcohol extract as an active ingredient. The anti-caries and anti-periodontal disease composition of the present invention has excellent anti-caries and anti-periodontal effects, and is effective against caries in young children who often eat sugar-containing foods, especially sweets and candy. It is extremely useful for preventing periodontal disease induced by dental caries and in adults. [Prior Art] Recent research has clarified that the two major diseases in the field of oral surgery, caries and periodontal disease, are both caused by oral bacteria. In particular, the oral bacterium Streptococcus mutans synthesizes sticky polysaccharide from sucrose in food and drink, and in the synthesized polysaccharide, various bacteria including Streptococcus mutans ( Lactic acid bacteria and gram-negative bacteria) multiply and finally form dental plaque, which can also be called bacterial flora. Furthermore, bacteria such as Streptococcus miutans produce organic acids such as lactic acid from various sugars, and these organic acids remain in dental plaque and attack the enamel layer, inducing caries. Furthermore, it is known that gram-negative bacterial toxins in dental plaque cause periodontal disease. Therefore, in order to prevent the occurrence of dental caries and periodontal disease, it is necessary to use bacteria that cause plaque formation. The most effective method is to inhibit the proliferation of Streptococcus miutans. In the past, several bactericidal agents or antibiotics have been studied to suppress the colonization of Streptococcus miutans in the oral cavity (Shigeyuki Hamada, "How does tooth decay occur?" February 22, 1982, Iwanami Shinsho P125-P133). There are also reports on oral cleaning compositions that utilize the antibacterial properties of some germ extracts (JP-A-57-56415, 1982-39615, 1983-
260012). However, each of these techniques has drawbacks and does not necessarily provide satisfactory results. In other words, conventional disinfectants such as antibiotics are not suitable for long-term use, and they indiscriminately kill oral bacteria, disrupting the balance of the normal flora and causing bacterial replacement. In addition, it often causes undesirable conditions, such as sometimes affecting intestinal bacteria. On the other hand, the effective plant extracts that have been reported are unsuitable for industrial production because their raw materials are herbal medicines or flavorings, which are difficult to obtain in large quantities and are expensive. [Problems to be solved by the invention] The present inventors have conducted intensive research to find a substance that exhibits antibacterial activity specifically against Treptococcus miutans and is highly safe for long-term use. We found that the ethyl acetate-soluble fraction of tea water or alcohol extracts that we drink daily has excellent anti-caries and anti-bacterial periopathic activities. [Means for Solving the Problems] The present inventors have developed a highly safe and excellent anti-caries and anti-periodontal composition containing an ethyl acetate soluble fraction of tea water or alcohol extract as an active ingredient. succeeded in obtaining. Tea in the present invention (Camellia sinensis, (L.)
0.Kuntze) refers to the whole tea plant or a part thereof, such as leaves, xylem, roots, fruits, etc., fresh or dried, as is, partially fermented products, and completely fermented products, and refers to each or a mixture thereof. Either can be used. First, extract the tea with a sufficient amount of water or alcohol. After extraction, the residue is separated by a known method to obtain an extract. The solvent was distilled off from the extract, the residue was dissolved in water, and then partitioned using hexane, chloroform, and ethyl acetate sequentially to obtain a hexane-soluble fraction, a chloroform-soluble fraction, and the desired ethyl acetate. Obtain each soluble fraction. The partitioning with hexane and chloroform in this operation can be omitted depending on the coloring degree and viscosity of the water or alcohol extract, but in order to increase the purity of the ethyl acetate soluble fraction, the partitioning with hexane and chloroform is necessary. It is desirable to implement the following. The temperature and time during extraction are not particularly limited, and the most efficient conditions may be selected for each condition. For example, 1 to 7 days is sufficient at room temperature, and 1 to 5 hours is sufficient at 60° C. or higher. As the alcohol used for extraction, lower alcohols such as methyl alcohol, ethyl alcohol, n-propyl alcohol, isopropyl alcohol, and butyl alcohol are preferred from the viewpoint of operability and extraction efficiency. Although the composition of this ethyl acetate soluble fraction has not yet been elucidated in detail, inorganic fluorine compounds have been reported as anti-caries components of tea (Kenjiro Ikegaya, Food and Development, vo1122, No.3.P22) They have different chemical components, and their effects were completely unknown, and their properties have been clarified for the first time through the present invention. [Effect] The anti-caries and anti-periodontal disease composition of the present invention showed extremely excellent results in an antibacterial test against the oral bacterium Streptococcus miutans.
These effects useful for preventing dental caries and periodontal disease will be explained in detail below using test examples. Test example Measurement of antibacterial activity Add 5 ml of Brain Heart Infusion (BHI) medium to a test tube, autoclave at 120°C for 15 minutes, add 100μ of a sample solution dissolved in methyl alcohol to this, and add 24 to 48 μl of the sample solution dissolved in methyl alcohol. Add 100μ of a suspension of the following bacteria that has been cultured for an hour, and culture the suspension at 37°C. Sample in BHI medium

【table】

[Table] Streptococcus miutans
RIMD 3125001

[Table] Streptococcus miutans
MT8148

【table】

[Table] Streptococcus miutans
6715DP

[How to use]

In order to use the ethyl acetate soluble fraction of the tea extract of the present invention as a composition for preventing dental caries or periodontal disease, it is preferable to use it as a suitable oral preparation. Such oral preparations may be in the form of liquids, solids, or semi-solids, and preferred preparations include toothpastes, gargles, lozenges, gargles, liquid coatings, and chewing gum. The excipients or auxiliary agents used to produce these oral preparations may be appropriately selected from those normally used for this type of purpose depending on the dosage form, and are not particularly limited. However, for example, lactose starch, corn starch, magnesium stearate, dicalcium phosphate dihydrate, sorbitol, carboxymethylcellulose, sodium saccharin lauryl sulfate, glycerin, sodium carboxymethylcellulose, silicic anhydride, gelatin, titanium dioxide, Menthol, fatty acids, citric acid, polyethylene glycol, sodium lauroyl sarcosinate, calcium carbonate, alcohol, carrageenan, sodium acyl taurate,
Peptone, gum arabic, lauryl diethanolamide, etc. are used. It is also possible to further enhance the caries prevention effect by adding fluorides such as sodium fluoride and sodium phosphate fluoride to the above preparation.
Sodium chloride, preservatives, flavoring agents, coloring agents, etc. may also be added as appropriate. The amount of ethyl acetate soluble fraction in oral preparations for caries prevention or periodontal disease prevention that can be produced in this way varies depending on the dosage form, but is usually about 0.01% by weight (weight/weight). ) or higher is desirable. [Example] Next, the present invention will be explained in detail with reference to Examples, but the present invention is not limited thereto. Example 1 Approximately 3 methanol was added to 500 g of commercially available green tea, stirred occasionally, and extracted at a constant temperature for 3 days. The extract was filtered to separate the methanol layer. Methanol was distilled off and the residue was dried to obtain 149 g of a deep green extract.
Five times the amount of water was added to the obtained extract to dissolve it, 3 portions of hexane was added, the mixture was vigorously stirred, and then allowed to stand overnight. The hexane layer was separated, distilled off, and dried to obtain 51 g of hexane soluble fraction. After adding chloroform 5 to the hexane-insoluble aqueous layer and stirring vigorously,
It was left undisturbed overnight. After separating and distilling off the chloroform layer,
After drying, 7.5 g of a chloroform-soluble fraction was obtained.
Ethyl acetate 5 was added to the chloroform-insoluble aqueous layer, stirred vigorously, and then allowed to stand overnight. The ethyl acetate layer was separated, evaporated, and dried to obtain 50 g of the desired ethyl acetate soluble fraction. Example 2 About 5 g of water was added to 300 g of commercially available karigane tea, stirred occasionally, and extracted at 60° C. for 3 hours. The extract was filtered and the aqueous layer was separated. Hexane 3 was added to the obtained aqueous layer, stirred vigorously, and then allowed to stand overnight. The hexane layer was separated, evaporated and dried to obtain 25 g of hexane soluble fraction. Chloroform 4 was added to the aqueous layer after hexane separation, and after stirring vigorously, it was allowed to stand overnight. The chloroform layer was separated, evaporated and dried to obtain 5.2 g of chloroform-soluble fraction. Ethyl acetate (3) was added to the aqueous layer after separation from chloroform, and the mixture was stirred vigorously and then allowed to stand overnight. Separate the ethyl acetate layer, evaporate and dry to obtain the desired ethyl acetate soluble fraction 21
I got g. Example 3 Dentifrice Dibasic calcium phosphate 42 Glycerin 19 Carrageenan 0.9 Sodium lauryl sulfate 1.2 Satucalin 1.0 Ethyl acetate soluble fraction of tea extract 1.0 Butyl paraoxybenzoate 0.005 Flavor 1.0 Water Total remaining amount 100 (wt%) Above components Manufactured using conventional methods for toothpaste. That is, the prescribed amounts of water, glycerin, carrageenan, saccharin, ethyl acetate soluble fraction of tea extract, butyl paraoxin benzoate, and fragrance are measured and mixed to swell the binder, and then the remaining ingredients are mixed. Add and mix further. After defoaming and mixing, fill the tube. [Effects of the Invention] The ethyl acetate soluble fraction of tea water or alcohol extract has a strong effect on Streptococcus miutans, which is the main causative bacterium that produces dental plaque that causes caries and periodontal disease. , exhibiting strong antibacterial activity. Tea, the raw material used in the present invention, has been used for drinking since ancient times, is highly safe, easily available, and is a practically appropriate raw material, and the method for obtaining the substance of the present invention is Since the method is extremely simple and can be operated in large quantities, the present invention makes it possible to supply highly effective anti-caries and anti-periodontal disease compositions in large quantities at low cost, contributing to the improvement of oral hygiene. Of course, it is also considered to be extremely useful industrially.

Claims (1)

[Scope of Claims] 1. An anti-caries and anti-periodontal disease composition containing an ethyl acetate soluble fraction of tea extract as an active ingredient. 2. The anti-caries and anti-periodontal disease composition according to claim 1, wherein the tea extract is a water or alcohol extract.